α7 nachr

SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.

CP-810123 is a new alpha 7 nAChR agonist for the treatment of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease.

Methyllycaconitine citrate (MLA) is an α7 neuronal nicotinic acetylcholine receptor (α7nAChR) antagonist that crosses the blood-brain barrier.

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

GTS-21 (DMXB-A) is an α7 nAChR agonist. GTS-21 suppresses inflammation associated with rheumatoid arthritis by inhibiting RA Th1 cell differentiation.

SSR180711 hydrochloride (SSR-180711A HCl) is a selective Alpha7 nicotinic acetylcholine partial agonist for the study of neurodegenerative and cognitive disorders.

PHA 543613 is a specific agonist of α7 nAChR (Ki = 8.8 nM) and can be used in studies about the cognitive deficits of Alzheimer's disease and schizophrenia.

TC-2216 is a partial agonist at the neural nicotinic acetylcholine receptor and is used to treat anxiety and depression.

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.

Cynandione A, an acetophenone derived from Cynanchum wilfordii, has anti-inflammatory activity and significantly reduces pro-inflammatory cytokine overexpression via macrophage α7 nAChR activation and subsequent IL-10 expression.

GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.

Benzethonium chloride (Quatrachlor) is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties.

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

PNU-282987 S enantiomer free base is an agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR).

AQW051 (VQW-765) is an orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) specific activator that interacts with recombinant human α7-nAChR expression (pKD value 7.56). Alpha7-nachr is considered an attractive target for the treatment of cognitive impairments associated with neurological disorders, so VQW-051 is often used in studies of anxiety disorders and acute anxiety.

A-582941 is a alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.

Pozanicline hydrochloride is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline hydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant[2].

S 24795 (Catestatin acetate(142211-96-9 free base)) is an α7 nAChR partial agonist. S 24795 improves mnemonic function in aged mice and can be used in studies about aging-related memory disturbances.

4BP-TQS is an allosteric agonist of α7 nAChRs.

neuronal α7 nAChR antagonist

High affinity α7 nAChR partial agonist (Ki = 1.1 nM in rat; Emax < 10% of the response to ACh in rat and human). Inhibits ACh (IC50 = 2.7 nM) at α7 nAChR. Reduces LPS-induced TNF-α release from microglia enriched cultures. Anti-inflammatory. Briggs et al (2009) Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors. Br.J.Pharmacol. 158 1486 PMID:19845675 |Thomsen et al (2012) The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J.Neuroimmunol. 251 65 PMID:22884467 |Papke et al (2015) The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor. Neuropharmacology 91 34 PMID:25497451